azd-0364

Description: AZD0364 is a potent and selective oral inhibitor of ERK1/2 that is efficacious in both monotherapy and combination therapy in models of NSCLC. It has an IC50 of 0.6 nM for ERK2. AZD0364 exhibits high cellular potency against a direct substrate (e.g., inhibition of phosphorylation of p90RSK in BRAF mutant A375 cells, IC50 = 6 nM) and is highly selective (10/329 kinases tested are inhibited at > 50% at 1 uM). In an unbiased cell proliferation screen of 750 tumor cell lines, > 50% of cell lines that are sensitive to AZD0364 have RAS/MAPK pathway genetic alterations such as BRAF, NRAS or KRAS mutations. In a subset of KRAS mutant NSCLC cell lines, combined treatment of AZD0364 and selumetinib (AZD6244, ARRY-142886) is highly synergistic.

References: Cancer Research 78(13 Supplement):1856-1856 DOI: 10.1158/1538-7445.AM2018-1856; WO2017080979A1.

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